Preparation of phytantriol cubosomes by solvent precursor dilution for the delivery of protein vaccines

Rizwan, Shakila B.; Assmus, D; Boehnke, Adam; Hanley, Tracey; Boyd, Ben J.; Rades, Thomas; Hook, Sarah

doi:10.1016/j.ejpb.2010.12.034

Cited by 149 publications

(106 citation statements)

References 33 publications

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“…The cubosomes of the former dispersion (E-F8) were prepared by the fragmentation method and could be seen as more or less cubic nanoparticles ( Figure 7A and B). On contrary, the liquid precursor-derived cubosomes were larger and showed structures with more circular edges ( Figure 7C and D) (Spicer & Hayden, 2001;Esposito et al, 2003;Rizwan et al, 2011). The appearance of multiple black dots within cubosomes was previously attributed to the presence of internal water channels (Madheswaran et al, 2014).…”

Section: In Vitro Characterization Of Enteric Surface-coated Cubosomamentioning

confidence: 93%

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

et al. 2016

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Context: Pravastatin sodium (PVS) is a freely water-soluble HMG-CoA inhibitor that suffers from instability at gastric pH, extensive first pass metabolism, short elimination half-life (1-3 h) and low oral bioavailability (18%). Objective: To overpower these drawbacks and to maximize drug absorption at its main site of absorption at the duodenum, enteric surface-coated PVS-loaded nanocubosomal dispersions were presented. Materials and methods: Glyceryl monooleate (GMO)-based dispersions were developed by the fragmentation or the liquid precursor methods using Pluronic Õ F127 or Cremophor Õ EL as surfactants. As a challenging entericcoating approach, the promising dispersions were surface-coated via lyophilization with Eudragit Õ L100-55; a duodenum-targeting polymer. The drug content, particle size, zeta potential, morphology and release studies of PVS-loaded dispersions were evaluated before and after surface-coating. Compared to an aqueous PVS solution, the pharmacokinetics of the best achieved system (E-F8) was evaluated (UPLC-MS/MS) in rats. Results: The enteric surfacecoated nanocubosomal dispersions were more or less spherical in shape and showed high drug-loading, negative zeta potential values and fine-tuned biphasic drug-release patterns characterized by retarded (2 h) and sustained (10 h) phases in pH 1.2 and pH 6.8, respectively. E-F8 system showed significantly (p50.05) higher oral bioavailability, delayed T max and prolonged MRT 0À1 following oral administration in rats. Conclusions: The duodenum-triggering potential and the controlled-release characteristics of the best achieved system for smart PVS delivery were revealed.

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Section: In Vitro Characterization Of Enteric Surface-coated Cubosomamentioning

confidence: 93%

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

et al. 2016

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“…10,11 Recently, using cubosomes as novel nanocarriers for protein molecules has garnered considerable interest due to their high encapsulation ability, which results in enhanced protein concentration on target sites. [12][13][14][15] Our previous work demonstrated that cubosomes stabilize the earthworm fibrinolytic enzyme -a model protein. This, in turn, enhances inner ear bioavailability after intratympanic injection.…”

Section: Introductionmentioning

confidence: 99%

Enhanced bioavailability of nerve growth factor with phytantriol lipid-based crystalline nanoparticles in cochlea

Tang

Wei

et al. 2015

IJN

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Purpose Supplementation of exogenous nerve growth factor (NGF) into the cochlea of deafened animals rescues spiral ganglion cells from degeneration. However, a safe and potent delivery of therapeutic proteins, such as NGF, to spiral ganglion cells remains one of the greatest challenges. This study presents the development of self-assembled cubic lipid-based crystalline nanoparticles to enhance inner ear bioavailability of bioactive NGF via a round window membrane route. Methods A novel nanocarrier-entrapped NGF was developed based on phytantriol by a liquid precursor dilution, with Pluronic ® F127 and propylene glycol as the surfactant and solubilizer, respectively. Upon dilution of the liquid lipid precursors, monodispersed submicron-sized particles with a slight negative charge formed spontaneously. Results Biological activity of entrapped NGF was assessed using pheochromocytoma cells with NGF-loaded reservoirs to induce significant neuronal outgrowth, similar to that seen in free NGF-treated controls. Finally, a 3.28-fold increase in inner ear bioavailability was observed after administration of phytantriol lipid-based crystalline nanoparticles as compared to free drug, contributing to an enhanced drug permeability of the round window membrane. Conclusion Data presented here demonstrate the potential of lipid-based crystalline nanoparticles to improve the outcomes of patients bearing cochlear implants.

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“…19 As shown in Figure 2B, the LCNPs constructed showed a bimodal polydispersed population with two distribution peaks (around 100 nm and 25 nm) and relative wide size distributions (polydispersity index 0.360-0.380). The particle distribution pattern was confirmed by our transmission electron microscopy data (Figure 2A), in which quite a few small particles (around 20 nm) were observed in the LCNP formulation.…”

Section: Discussionmentioning

confidence: 99%

“…19 Soy phosphatidylcholine, glycerol dioleate, and polysorbate 80, with or without paclitaxel, were mixed with the hydrotrope (10% ethanol to total additives, w/w) and stirred for 3 hours to form a uniform and clear oil phase. HEPES (N′-a-hydroxythylpiperazine-N′-ethanesulfanic acid) solution (containing 20 mM HEPES, pH 7.4, 20% to lipid, w/w) was gently added to the oil phase.…”

Section: Preparation Of Lcnpsmentioning

confidence: 99%

Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption

Zeng¹,

Gao²,

Hu³

et al. 2012

IJN

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Background: Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as novel drug-delivery systems for improving the bioavailability of both hydrophilic and hydrophobic drugs. However, their cellular interaction and in vivo behavior have not been fully developed and characterized. Methods: In this study, self-assembled LCNPs prepared from soy phosphatidylcholine and glycerol dioleate were developed as a platform for oral delivery of paclitaxel. The particle size of empty LCNPs and paclitaxel-loaded LCNPs was around 80 nm. The phase behavior of the liquid crystalline matrix was characterized using crossed polarized light microscopy and small-angle X-ray scattering, and showed both reversed cubic and hexagonal phase in the liquid crystalline matrix. Transmission electron microscopy and cryofield emission scanning electron microscopy analysis revealed an inner winding water channel in LCNPs and a "ball-like"/"hexagonal" morphology. Results: Cellular uptake of LCNPs in Caco-2 cells was found to be concentration-dependent and time-dependent, with involvement of both clathrin and caveolae/lipid raft-mediated endocytosis. Under confocal laser scanning microscopy, soy phosphatidylcholine was observed to segregate from the internalized LCNPs and to fuse with the cell membrane. An in vivo pharmacokinetic study showed that the oral bioavailability of paclitaxel-loaded LCNPs (13.16%) was 2.1 times that of Taxol ® (the commercial formulation of paclitaxel, 6.39%). Conclusion: The findings of this study suggest that this LCNP delivery system may be a promising candidate for improving the oral bioavailability of poorly water-soluble agents.

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Preparation of phytantriol cubosomes by solvent precursor dilution for the delivery of protein vaccines

Cited by 149 publications

References 33 publications

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

Duodenum-triggered delivery of pravastatin sodium: II. Design, appraisal and pharmacokinetic assessments of enteric surface-decorated nanocubosomal dispersions

Enhanced bioavailability of nerve growth factor with phytantriol lipid-based crystalline nanoparticles in cochlea

Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption

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